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UU / Semester-7 / Chapter-1 / Introduction/ A.

Samanta / 2005 1

Introduction to biopharmaceutics and pharmacokinetics
Introduction to biopharmaceutics and pharmacokinetics and their role in information development and clinical setting.

Definition of Biopharmaceutics
Biopharmaceutics can be defined as the study of the
interrelationship of the physicochemical properties of the drug,
the dosage form in which the drug is given,
and the route of administration
on the rate and extent (amount) of systemic drug absorption.

Thus biopharmaceutics deals with the factors that influence the

1. protection of the activity of the drug within the drug product (stability)
2. the release of the drug from the a drug product
3. the rate of dissolution of the drug at the absorption site, and
4. the systemic absorption of the drug.

Studies of biopharmaceutics involves both in-vitro and in-vivo methods.

In-vitro methods involves test apparatus without involving laboratory animals or humans. E.g. disintegration tests,
dissolution tests etc.
In-vivo test involves measurement of systemic drug availability (bioavailability) after giving a drug product to an
animal or human.

Drug in dosage form

Drug release

Drug at absorption site BIOPHARMA

PHARMACO Drug absorption
Drug in systemic circulation

Drug in extravascular tissues Metabolism DISPOSITION
Drug at site of action Excretion


In normal body
Pharmacologic response


In diseased body
Therapeutic effect at therapeutic dose
Toxic effect at toxic dose

Schematic representation of the process involved in drug therapeutics

UU / Semester-7 / Chapter-1 / Introduction/ A. Samanta / 2005 2

Pharmacokinetics is defined as the study of rate processes involved in absorption, distribution, metabolism and
excretion (ADME).
The study of pharmacokinetics involves both
experimental and theoretical approaches. Absorption Disposition
The experimental approach involves
1. the development of biological sampling Distribution Elimination
2. analytical methods development for the
measurement of drugs and metabolites Excretion Metabolism
3. and the procedures for data collection and manipulation.

The theoretical aspect of pharmacokinetics involves the development of pharmacokinetic models that predicts drug
disposition after drug administration.

The application of statistics is an integral part of pharmacokinetic models top determine data errors, deviation of
models and correlation.

Clinical pharmacokinetics is the application of pharmacokinetic methods in drug therapy.

This is a multidisciplinary approach where the dose of a drug is optimized for a specific patient depending on the
disease state, age and sex of the patient. This subject requires information from medical and pharmaceutical research.

Population pharmacokinetics is the study of pharmacokinetic differences of drug in various population groups.

Therapeutic drug monitoring (TDM)

When drug with narrow therapeutic indices are used in patients, it is necessary to monitor plasma drug concentration
closely by taking periodic blood samples. Some drugs those are frequently monitored are aminoglycoside antibiotics,
convulsants and anticancer drugs in order to minimize adverse side effects.

Pharmacodynamics deals with the relationship between the drug concentration at the site of action (receptor) and
pharmacologic response, including biochemical and physiological effects that influence the interaction of drug with the
Under pharmacodynamics we study the relationship between the plasma concentration of drug (related to the
concentration at the site of action) and the magnitude of biological effect it shows.

Toxicokinetics is the application of pharmacokinetic principles to the design, conduct and interpretation of drug safety
evaluation studies and used in validating dose related exposure in animals. Toxicokinetic studies are conducted in
animals and the result obtained is used to interpret possible toxic reactions in human.

The ultimate aim of a drug is to achieve optimal therapy.

1. To attain this aim the drug is first molded into a suitable dosage form.
2. The dosage form is administered in to the body through a suitable route of administration.
3. The drug is released at the site of absorption at a certain rate.
4. The drug is then absorbed from the site of absorption to systemic circulation.
5. The drug is carried to various tissues through blood. The drug is distributed to extravascular tissues. The
distribution method is a reversible process. The drug returns back to the systemic circulation.
6. The drug produces its action at the site of action. The site of action may reside in some extravascular tissues.
7. The drug is excreted through kidney and metabolize in the liver and various tissues. Thus the drug is eliminated
from the body.
All the above processes are occurring at a certain rate. Under the subject pharmacokinetics we study those rates and
built up equations to predict those rate processes.
UU / Semester-7 / Chapter-1 / Introduction/ A. Samanta / 2005 3

Application of biopharmaceutics
1. A company is going to market a new dosage form of a certain drug. The dose is known. When this dosage form is
administered to a healthy human the drug may not released quickly. In this case the action of the drug will be
delayed. In another case if the drug is released all at a time then the duration of action of the drug will be very
short. So with the knowledge of biopharmaceutics we can change various formulation factors to obtain optimum
onset of action and duration of action.
2. A company is marketing tablets of a certain drug. Now it wants to change a few ingredients or some formulation
factors. The new tablets may not behave similarly as the previous one. So the bioavailability of new tablets are
compared with the old tablets. If it is found that the bioavilability of the newer tablets are equivalent (i.e
bioequivalent) to that of older tablets then the new tablets will be permitted to market (by FDA).
3. A company is marketing the tablets of a certain drug. Now they have planned to make transdermal dosage form of
the same drug. To establish its efficacy the bioavailability of the transdermal dosage form is compared to that of
the established tablet dosage form. If both are found to be closer then the transdermal dosage form will be accepted
by FDA.

Application of pharmacokinetics
1. The bioavailabilty of a dosage form is calculated by pharmacokinetic equations.
2. The frequency of dosing is calculated from pharmacokinetic equations.
3. To calculate the dose of a controlled release dosage form pharmacokinetic equations are required.
4. In case of patients with kidney failure the dose of a drug should be calculated very cautiously. If the rate of
absorption of the drug is greater than the elimination rate of the drug from that patient then the drug will be
accumulated in the body and may show toxic effect. The rate of elimination of the drug from the body of that
patient is calculated with the help of pharmacokinetic equations.
5. When a potent anticancer drug is administered to a patient the plasma concentration of the drug must be very close
to minimum effective concentration. Since the therapeutic index of the drug is very narrow in case of potent drugs
so rate of administration must also be very slow. This rate of administration is calculated by pharmacokinetic